外消旋瑞格列奈的合成

Synthesis of Racemic Repaglinide

以 4-甲基水杨酸和 2 -氟苯甲醛为起始原料 ,采用 Ph3P催化缩合反应为关键步骤合成外消旋瑞格列奈 ,总收率 8.6 % .关键中间体及最终化合物的结构经元素分析、质谱。

Racemic repaglinide, (a new kind of antidiabetic drug), (±) 2 ethoxy 4 [2 ((3 methyl 1 [2 (1 piperidinyl)phenyl] butyl)amino) 2 oxoethyl]benzoic acid, was synthesized by employing Ph 3P catalytic condensation as a pivotal step The total yield was 8 6% The structures of the intermediates and the target molecule were confirmed by MS, elementary analysis, 1H NMR and 13 C NMR spectra in our experiments The route does not require high pressure and high temperature that may be applied to industrial production